公开(公告)号：US11352360B2

公开(公告)日：2022-06-07

申请号：US16360162

申请日：2019-03-21

Applicant: Rigel Pharmaceuticals, Inc. ,  Bristol-Myers Squibb Company

Inventor： Todd Kinsella ,  Marina Gelman ,  Hui Hong ,  Ihab S. Darwish ,  Rajinder Singh ,  Jiaxin Yu ,  Robert M. Borzilleri ,  Upender Velaparthi ,  Peiying Liu ,  Chetan Padmakar Dame ,  Hasibur Rahaman ,  Jayakumar Sankara Warrier

IPC: C07D487/04 ,  C07D401/04 ,  C07D403/04 ,  C07D471/04 ,  A61P35/00 ,  C07D417/04

Abstract: Disclosed are imidazole and thiazole compounds, as well as pharmaceutical compositions and methods of use thereof. One embodiment is a compound having the structure and pharmaceutically acceptable salts, prodrugs and N-oxides thereof (and solvates and hydrates thereof), wherein X, A, Z, R1 and R′ are as described herein. In certain embodiments, a compound disclosed herein inhibits TGF-β, and can be used to treat disease by blocking TGF-β signaling.

公开(公告)号：US20160311824A1

公开(公告)日：2016-10-27

申请号：US15034217

申请日：2014-11-14

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Upender Velaparthi ,  Chetan Padmakar Dame ,  Peiying Liu ,  Mark D Wittman ,  Bradley C. Pearce ,  Erika M.V. Araujo ,  Bireshwar Dasgupta ,  Jalathi Surendran Nair ,  Sakthi Kumaran Janakiraman ,  Chandrasekhar Reddy Rachamreddy ,  Mallikarjuna Rao Mettu ,  Arul Mozhi Selvan Subbiah Karuppiah ,  Bandreddy Subba Reddy ,  Pulicharla Nagalakshmi ,  Rajesh Onkardas Bora ,  Shilpa Holehatti Maheshwarappa ,  Selvakumar Kumaravel ,  Dibakar Mullick ,  Ramesh Sistla

IPC: C07D487/04 ,  C07D487/20 ,  C07D491/147 ,  C07D491/20 ,  C07D519/00 ,  C07D487/10

CPC classification number: C07D487/04 ,  C07D487/10 ,  C07D487/20 ,  C07D491/147 ,  C07D491/20 ,  C07D519/00

Abstract: The invention provides compounds of Formula (I): and pharmaceutically acceptable salts thereof. The compounds of Formula (I) inhibit protein kinase activity thereby making them useful as anticancer agents.

Abstract translation: 及其药学上可接受的盐。 式（I）的化合物抑制蛋白激酶活性，从而使它们用作抗癌剂。